Chemo-enzymatic cascade processes are invaluable due to their ability to rapidly construct high-value products from available feedstock chemicals in a one-pot relay manner. In an article, author is Koshizawa, Tomoaki, once mentioned the application of 10310-21-1, Name is 2-Amino-6-chloropurine, molecular formula is C5H4ClN5, molecular weight is 169.5718, MDL number is MFCD00075252, category is piperidines. Now introduce a scientific discovery about this category, HPLC of Formula: C5H4ClN5.
Discovery of novel spiro[chromane-2,4 ‘-piperidine] derivatives as potent and orally bioavailable G-protein-coupled receptor 119 agonists
Herein, we describe the discovery, synthesis, and evaluation of a novel series of spiro[chromane-2,4’-piperidine] derivatives as G-protein-coupled receptor 119 agonists. Their initial design exploited the conformational restriction in the linker-to-tail moiety, which was a key concept in this study, to give lead compound 11 (EC50 = 369 nM, E-max = 82%). An extensive structure-activity relationship study resulted in the identification of the optimized drug candidate (R)-29 (EC50 = 54 nM, E-max = 181%). The defining structural features of the series were a terminal benzyl-type bulky substituent and a methylene linker between the sulfonyl and phenyl groups, both of which were in the head moiety as well as the spiro-type scaffold in the linker-to-tail moiety. An in vivo oral glucose-tolerance test using C57BL/6N mice showed that (R)-29 reduced glucose excursion at a dose of 3 mg/kg in a dose-dependent manner.
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Reference:
Piperidine – Wikipedia,
,Piperidine | C5H11N – PubChem